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Insulin Glargine

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From Pharmacopedia
Insulin glargine
Lantus, Basaglar, Semglee, Toujeo (U-300)

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Summary
Common uses
Type 1 diabetes mellitus0, Type 2 diabetes basal coverage0
Pharmacy
Starting dose
~10 units SC at the same time daily, or 0.1-0.2 units/kg/d; titrate by fasting glucose
Preparations
100 U/mL (Lantus, Basaglar, Semglee) vials and pens; 300 U/mL (Toujeo) pens
US FDA Max
Titrated to glucose; no fixed ceiling
Pharmacology
Routes
Subcutaneous (never IV; not for use in insulin pumps)
Onset
1-2 hours
Duration
~24 hours per dose (peakless profile by design)
Half-life
~12 hours apparent (functional duration ~24 hours due to depot release kinetics)[1]
Bioavailability
~100% from subcutaneous depot (by definition of the route)
Pregnancy
Insulin is the preferred glucose-lowering therapy in pregnancy; glargine has reassuring observational data, though NPH and detemir remain the traditional choices.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Insulin glargine is a recombinant human insulin analog (Gly-A21, two added Arg residues at B-chain C-terminus) that precipitates as microcrystals at physiologic pH after injection from its acidic formulation, producing slow continuous redissolution and a near-peakless 24-hour basal insulin profile.0 Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio; provides basal hepatic glucose suppression and peripheral glucose uptake without prandial peaks[1].

References

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  1. 1.0 1.1 FDA Prescribing Information, Lantus (insulin glargine), Sanofi-Aventis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021081s063lbl.pdf